Method of reducing blood glucose
The present invention relates to the use of compounds of the general formula ##STR1## for reducing blood glucose and/or inhibit the secretion, circulation or effect of insulin antagonizing peptides like CGRP or amylin. Hence the compound can be used in the treatment of insulin resistance related to NIDDM (non-insulin-dependent diabetes mellitus) or aging.
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Claims
1. A method for reducing blood glucose and/or inhibiting the activity of CGRP comprising administering to a patient a clinically effective amount of a compound of formula I ##STR4## wherein R.sup.1 and R.sup.2 independently are hydrogen, halogen, trifluoromethyl, C.sub.1-6 -alkyl or C.sub.1-6 -alkoxy;
- Y is >N--CH.sub.2 --, >CH--CH.sub.2 -- or >C.dbd.CH-- wherein only the underscored atom participates in the ring system;
- X is --O--, --S--, CR.sup.7 R.sup.8, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--CH.sub.2 --, --CH.sub.2 --CH.dbd.CH--, --CH.sub.2 CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, NR.sup.9 (C.dbd.O)--, --O--CH.sub.2 --, --(C.dbd.O)-- or --(S.dbd.O)-- wherein R.sup.7, R.sup.8 and R.sup.9 independently are hydrogen or C.sub.1-6 -alkyl;
- r is 1, 2, or 3;
- m is 1 or 2;
- n is 1 when m is 1 and n is 0 when m is 2;
- R.sup.4 and R.sup.5 represents hydrogen or may--when m is 2--together represent a bond; and
- R.sup.6 is OH or C.sub.1-8 -alkoxy; or
2. The method according to claim 1 wherein R.sup.1 and R.sup.2 independently are hydrogen, halogen, triflouromethyl or methoxy.
3. The method according to claim 1 wherein Y is >N--CH.sub.2.
4. The method according to claim 3 wherein X is --O--, --S--, --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --CH.dbd.CH--, --N(CH.sub.3)(C.dbd.O)--, --O--CH.sub.2 --, --(C.dbd.O)-- or --(S.dbd.O)--.
5. The method according to claim 1 wherein Y is >C.dbd.CH--.
6. The method according to claim 5 wherein X is --O--, --S--, --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --CH.dbd.CH--, --N(CH.sub.3)(C.dbd.O)--, --O--CH.sub.2 --, --(C.dbd.O)-- or --(S.dbd.O)--.
7. The method according to claim 1 wherein X is --O--, --S--, --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --CH.dbd.CH--, --N(CH.sub.3)(C.dbd.O)--, --O--CH.sub.2 --, --(C.dbd.O)-- or --(S.dbd.O)--.
8. The method according to claim 1 wherein R.sup.6 is OH.
9. The method according to claim 1 wherein m is 1.
10. The method according to claim 1 wherein m is 2.
12. The method according to claim 1 wherein the compound is in a form suitable for oral administration.
13. The method according to claim 1 wherein the compound is administered at a dose in a range from about 0.5 to 1000 mg/day.
16. The method according to claim 1 wherein the compound is
- (R)-1-(3-(5-Oxo-10H-phenothiazin-10-yl)-1-propyl)-3-piperidinecarboxylic acid;
- (R)-1-(3-(10H-Phenoxazin-10-yl)-1-propyl)-3-piperidinecarboxylic acid; or
17. The method according to claim 1 wherein the compound is (R)-1-(3-(9(H)-Oxo-10H-acridin-10-yl)-1-propyl)-3-piperidinecarboxylic acid or a pharmaceutically acceptable salt thereof.
19. The method according to claim 1 wherein the compound is 1-(3-(Thioxanthen-9-ylidene)-1-propyl)-3-piperidinecarboxylic acid or a pharmaceutically acceptable salt thereof.
3177211 | April 1965 | Zenitz et al. |
WO 92/06954 | April 1992 | WOX |
WO 92/16226 | October 1992 | WOX |
WO 95/18793 | July 1995 | WOX |
Type: Grant
Filed: Dec 13, 1996
Date of Patent: Apr 21, 1998
Assignee: Novo Nordisk A/S (Bagsvaerd)
Inventor: Uffe Bang Olsen (Vallensbaek)
Primary Examiner: Marianne M. Cintins
Assistant Examiner: Dwayne C. Jones
Attorneys: Steve T. Zelson, Esq., Eliass J. Lambiris, Esq.
Application Number: 8/766,839
International Classification: A01N 4346; A61K 3155;